Hepatocellular Carcinoma (HCC) Medication

Updated: Nov 25, 2019
  • Author: Luca Cicalese, MD, FACS; Chief Editor: John Geibel, MD, MSc, DSc, AGAF  more...
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Medication

Medication Summary

Few systemic options exist for patients with hepatocellular carcinoma (HCC). Sorafenib, regorafenib, nivolumab, lenvatinib, pembrolizumab, cabozantinib, and ramucirumab are the most recent options for patients with unresectable or advanced HCC.

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Antineoplastics, Tyrosine Kinase Inhibitor

Class Summary

Tyrosine kinase inhibitors have shown inhibitory activity of membrane-bound and intracellular kinases involved in normal cellular functions and in pathological processes.

Sorafenib (Nexavar)

Sorafenib is a tyrosine kinase inhibitor. It is indicated for unresectable hepatocellular carcinoma.

Regorafenib (Stivarga)

Regorafenib is a tyrosine kinase inhibitor. It is indicated for hepatocellular carcinoma in patients who have been previously treated with sorafenib.

Cabozantinib (Cabometyx)

Cabozantinib is an inhibitor of multiple tyrosine kinases, including RET, MET, and VEGFR-2. It is indicated for HCC in patients previously treated with sorafenib.

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Antineoplastics, VEGF Inhibitor

Class Summary

Inhibits the kinase activities of various subtypes of vascular endothelial growth factor (VEGF) receptors.

Lenvatinib (Lenvima)

Lenvatinib is a receptor tyrosine kinase (RTK) inhibitor that inhibits the kinase activities of VEGFR1 (FLT1), VEGFR2 (KDR), and VEGFR3 (FLT4). It also inhibits other RTKs that have been implicated in pathogenic angiogenesis, tumor growth, and cancer progression in addition to their normal cellular functions, including fibroblast growth factor (FGF) receptors FGFR1, 2, 3, and 4; the platelet-derived growth factor receptor alpha (PDGFR-α); KIT; and RET. It is indicated for first-line treatment of unresectable HCC.

Ramucirumab (Cyramza)

Vascular endothelial growth factor receptor 2 (VEGFR2) antagonist that specifically binds VEGF receptor 2 and blocks binding of VEGFR ligands, VEGF-A, VEGF-C, and VEGF-D. As a result, ramucirumab inhibits ligand-stimulated activation of VEGF2, thereby inhibiting ligand-induced proliferation, and migration of human endothelial cells. It is indicated as monotherapy for hepatocellular carcinoma (HCC) in patients with alpha fetoprotein (AFP) of 400 ng/mL or higher who have been previously treated with sorafenib.

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PD-1/PD-L1 Inhibitors

Class Summary

PD-1 and related target PD-ligand 1 (PD-L1) are expressed on the surface of activated T cells under normal conditions. PD-L1/PD-1 interaction inhibits immune activation and reduces T-cell cytotoxic activity when bound.

Nivolumab (Opdivo)

Nivolumab is a programmed death receptor-1 (PD-1) blocking antibody. It is indicated for hepatocellular carcinoma in patients who have been previously treated with sorafenib.

Pembrolizumab (Keytruda)

Pembrolizumab is a monoclonal antibody that binds to the PD-1 receptor and blocks its interaction with PD-L1 and PD-L2, releasing PD-1 pathway-mediated inhibition of the immune response, including the antitumor immune response. Binding of PD-1 ligands, PD-L1 and PD-L2, to the PD-1 receptor found on T cells, inhibits T cell proliferation and cytokine production. It is indicated for patients with hepatocellular carcinoma (HCC) who have been previously treated with sorafenib.

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